rocbrutinib (LP-168) / Lupeng Pharma, Jiangsu Hansoh Pharma - LARVOL DELTA

A Study of Rocbrutinib Combined With R-GemOx in Patients With Relapsed or Refractory Diffuse Large B-cell Lymphoma (clinicaltrials.gov) - P1 | N=42 | Recruiting | Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD. | Not yet recruiting ➔ Recruiting

Enrollment open • B Cell Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

First Report of a Phase Ib Study of Rocbrutinib, a Fourth-Generation Bruton's Tyrosine Kinase Inhibitor, Combined with R-CHOP in Patients with Previously Untreated B-Cell Lymphoma (ESMO 2026) - No abstract available

Clinical • P1 data • B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

LP-168-CN101: A Study of LP-168 in Participants With Relapse or Refractory B-Cell Lymphoma (clinicaltrials.gov) - P1 | N=200 | Recruiting | Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD. | Trial completion date: Jun 2027 ➔ Sep 2027 | Trial primary completion date: Dec 2026 ➔ Mar 2027

Trial completion date • Trial primary completion date • B Cell Lymphoma • Chronic Lymphocytic Leukemia • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

LP-168-CN301: Phase Ib Study of Rocbrutinib in Combination With R-CHOP in Patients With Newly Diagnosed B-cell Non-Hodgkin Lymphoma (clinicaltrials.gov) - P1 | N=112 | Active, not recruiting | Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD. | Recruiting ➔ Active, not recruiting | Trial primary completion date: Dec 2025 ➔ Jun 2027

Enrollment closed • Trial primary completion date • B Cell Non-Hodgkin Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Physiologically Based Pharmacokinetic Modeling to Predict Human Starting Dose and Pharmacokinetics for Rocbrutinib. (PubMed, Clin Transl Sci) - "Moreover, the predicted brain BTK occupancy at 12.5 mg was approximately 37% for wild-type BTK and 6% for C481S mutant BTK. The PBPK model serves as a valuable tool for dose selection, PK prediction, and CNS target engagement evaluation, supporting the clinical development of rocbrutinib."

Journal • PK/PD data

A Study of Rocbrutinib in PRL-Positive Relapsing-Remitting Multiple Sclerosis (clinicaltrials.gov) - P2 | N=30 | Recruiting | Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD.

New P2 trial • CNS Disorders • Multiple Sclerosis

A Study of Rocbrutinib in Combination With Lacutoclax in Patients With B-Cell Malignancies (clinicaltrials.gov) - P1/2 | N=92 | Recruiting | Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD. | Not yet recruiting ➔ Recruiting

Enrollment open • B Cell Lymphoma • Diffuse Large B Cell Lymphoma • Follicular Lymphoma • Hematological Malignancies • Lymphoma • Mantle Cell Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Rocbrutinib, a Highly Selective Fourth-Generation Covalent and Noncovalent BTK Inhibitor, in R/R Non-GCB DLBCL: Efficacy and Safety from a Phase I Study. (PubMed, Adv Ther) - P1 | "Rocbrutinib demonstrated promising efficacy and favorable tolerability profile in heavily pre-treated R/R non-GCB DLBCL. A 200 mg QD dose was selected as recommended phase 2 dose for monotherapy. A randomized phase II clinical trial in this population is currently enrolling."

Journal • P1 data • Atrial Fibrillation • B Cell Lymphoma • Cardiovascular • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

ROCKET-CLL: A RANDOMIZED, OPEN-LABEL, MULTICENTER, PHASE 3 STUDY OF ROCBRUTINIB (LP-168) VERSUS PIRTOBRUTINIB IN COVALENT BTK INHIBITOR (CBTKI) PRETREATED RELAPSED OR REFRACTORY (R/R) CLL/SLL (EHA 2026) - P1, P3 | "Exploratory endpoints include health- related quality of life and biomarker assessment. Recruitment is ongoing."

Clinical • IO biomarker • P3 data • Chronic Lymphocytic Leukemia • Small Lymphocytic Lymphoma • TP53

FIRST REPORT OF ROCBRUTINIB FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY PRIMARY CENTRAL NERVOUS SYSTEM LYMPHOMA (EHA 2026) - P1 | "Methods In this open-label phase 1 study, eligible subjects had a PCNSL diagnosis and had received at least one prior therapy, including a high- dose methotrexate-based regimen; prior BTKi exposure was permitted, including patients who were refractory to covalent BTKi. These findings support its potential for treating R/R PCNSL. Baseline Characteristics and Waterfall Plot of Subjects with R/R PCNSL"

Clinical • B Cell Lymphoma • CNS Lymphoma • Diffuse Large B Cell Lymphoma • Dyslipidemia • Hematological Malignancies • Hypertriglyceridemia • Lymphoma • Non-Hodgkin’s Lymphoma • Primary Central Nervous System Lymphoma • BTK

EFFECT OF A STRUCTURED, SEMI-SUPERVISED EXERCISE INTERVENTION IN CHRONIC LYMPHOCYTIC LEUKEMIA (CLL): FITNESS, CLINICAL OUTCOMES, AND CIRCULATING IMMUNE REPERTOIRE (EHA 2026) - "Further nonlinear regression and extra sum-of-squares F test analysis showed significant differences in killing curves between E0 and after EX12 (acalabrutinib p =0.0021, venetoclax p =0.039, ibrutinib p =0.025, rocbrutinib p =0.038) indicating enhanced drug sensitivity after EX12. Clinical implications of exercise-induced immune mobilization in CLL warrant further investigation. *contributed equally"

Clinical • Clinical data • Chronic Lymphocytic Leukemia • Hematological Malignancies • Infectious Disease • Leukemia • NCAM1 • TP53

UPDATED EFFICACY AND SAFETY RESULTS OF ROCBRUTINIB FROM THE PHASE 2 ROCK-1 STUDY IN PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA AND PREVIOUSLY TREATED WITH BTK INHIBITOR (EHA 2026) - P2, P3 | "Summary/Conclusion With extended follow-up, rocbrutinib still showed durable efficacy and favorable safety in patients with R/R MCL. A randomized phase 3 confirmatory trial of rocbrutinib versus investigator's choice of BTK inhibitors in patients with R/R MCL is ongoing (NCT07377578)."

Clinical • P2 data • Atrial Fibrillation • Cardiovascular • Constipation • Gastroenterology • Gastrointestinal Disorder • Hematological Disorders • Hematological Malignancies • Infectious Disease • Leukopenia • Lymphoma • Mantle Cell Lymphoma • Neutropenia • Pneumonia • Respiratory Diseases • Solid Tumor • Thrombocytopenia • Uterine Leiomyoma

NOVEL THERAPIES FOR RELAPSED/REFRACTORY MANTLE CELL LYMPHOMA POST BRUTON'S TYROSINE KINASE INHIBITOR: A TARGETED LITERATURE REVIEW (ISPOR 2026) - "Five ongoing studies without outcomes reported are evaluating ixazomib, odronextamab, and rocbrutinib...Drugs evaluated included antibody-drug conjugates (ADCs) (zilovertamab, polatuzumab + obinutuzumab), bispecific antibodies (BsAbs) (mosunetuzumab-based, glofitamab), noncovalent BTKi (ncBTKi) (pirtobrutinib), chimeric antigen receptor T-cell (CAR-T) (brexucabtagene, lisocabtagene, tisagenlecleucel), ViPOR regimen (venetoclax, ibrutinib, prednisone, obinutuzumab, and lenalidomide), proteasome inhibitor (PI) (carfilzomib)... Preliminary data indicate promising but heterogenous results within drug classes. Interpretation is limited by small sample sizes and differences in study design, underscoring the need for further investigation in this area of high unmet need."

Review • Hematological Malignancies • Lymphoma • Mantle Cell Lymphoma

ROCK-2: An ongoing open-label, randomized, multicenter phase 2 study of rocbrutinib versus investigator's choice of therapy in patients with R/R non-GCB DLBCL. (ASCO 2026) - P2 | "The BR regimen consists 6 cycles of rituximab (375 mg/m² on day 1) plus bendamustine (90 mg/m²/d on days 1-2). The R2 regimen consists of rituximab (375 mg/m² on day 1 of cycles 1-6) plus lenalidomide (20 mg QD on days 1-21 of each 28d-cycle until disease progression or unacceptable toxicity)...Recruitment is ongoing. ClinicalTrials.gov Identifier: NCT07189065."

Clinical • P2 data • B Cell Lymphoma • Diffuse Large B Cell Lymphoma • Indolent Lymphoma • Infectious Disease

MODULE 4: Selection and Sequencing of Therapy for R/R CLL (ASCO 2026) - "Supported by This activity is supported by educational grants from AstraZeneca Pharmaceuticals LP and Eli Lilly. Clinical and biological factors guiding decision-making for patients with R/R CLL; impact of the evolving up-front CLL treatment paradigm on the management of R/R disease Long-term follow-up from Phase III trials evaluating covalent BTK inhibitors and Bcl-2 inhibitors for patients with R/R CLL; current role of rechallenge with an agent or class of agents received in a prior line of therapy Published findings from key trials, such as BRUIN and BRUIN CLL-321, supporting the use of pirtobrutinib for patients with R/R CLL Emerging positive findings from the Phase III BRUIN CLL-322 trial of pirtobrutinib in combination with venetoclax and rituximab versus venetoclax and rituximab for patients with R/R CLL Available and emerging efficacy and safety data with and ongoing evaluation of other noncovalent BTK inhibitors, such as nemtabrutinib and rocbrutinib, for R/R..."

Chronic Lymphocytic Leukemia

Novel BTK inhibitors and degraders for relapsed/refractory CLL/SLL: latest updates from ASH 2025 annual meeting. (PubMed, J Hematol Oncol) - "Phase 1 studies of docirbrutinib and rocbrutinib demonstrated target engagement across wild-type and resistance-associated BTK mutations with encouraging safety profiles and preliminary efficacy signals in heavily pretreated populations...BTK degraders, including bexobrutideg and BGB-16673, demonstrated rapid and deep responses, activity in high-risk molecular subgroups, and manageable toxicity profiles, with recommended phase 2 doses established. Collectively, these latest updates support continued clinical development of novel agents to address resistance and disease progression in R/R CLL/SLL."

IO biomarker • Journal • Chronic Lymphocytic Leukemia • Hematological Disorders • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma • LYN

A Phase Ib/II Study of Rocbrutinib in Combination With Lacutoclax in Patients With B-Cell Malignancies (clinicaltrials.gov) - P1/2 | N=92 | Not yet recruiting | Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD.

New P1/2 trial • B Cell Lymphoma • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Follicular Lymphoma • Hematological Malignancies • Leukemia • Lymphoma • Lymphoplasmacytic Lymphoma • Mantle Cell Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma • Waldenstrom Macroglobulinemia

Guangzhou Lupeng/Newave Pharmaceutical Inc. Enrolled the First Patient in the Global Phase 3 ROCKET-CLL Trial Evaluating Rocbrutinib (LP-168) vs. Pirtobrutinib in R/R CLL/SLL (The Manila Times) - "This head-to-head study evaluates the efficacy and safety of rocbrutinib (LP-168), a novel oral fourth-generation BTK inhibitor, against pirtobrutinib in patients with relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (R/R CLL/SLL) who have received prior therapy with a covalent BTK inhibitor (cBTKi)...The first study site of the ROCKET-CLL Phase 3 trial (LP-168-US-CLL301; NCT07342478) was activated on April 28, 2026, at OptumCare Cancer Care Center in Las Vegas, Nevada, under the leadership of Dr. Russell Gollard...ROCKET-CLL is a randomized, open-label, multicenter Phase 3 study expected to enroll approximately 306 adult patients worldwide....Enrollment is expected to be completed by early Q4 2027, with an interim analysis planned for 2029."

Enrollment status • P3 data • Chronic Lymphocytic Leukemia • Small Lymphocytic Lymphoma

Lupeng Pharmaceutical's BTK inhibitor is planned to be included in the priority review [Google translation] (PhIRDA) - "On May 8, the official website of the Center for Drug Evaluation (CDE) of the China National Medical Products Administration announced that the rocbrutinib tablets applied by Lupeng Pharmaceuticals are planned to be included in the priority review, which is suitable for adult mantle cell lymphoma (MCL) patients who have previously received Bruton's tyrosine kinase (BTK) inhibitor treatment....Based on the safety and efficacy data of LP-168 obtained in the Phase 1 study, the CDE agreed to use the ROCK-1 study as a pivotal registration study to support the conditional marketing application of LP-168 in the target population."

China filing • Priority review • Mantle Cell Lymphoma

Lupeng Pharmaceutical today announced that the National Medical Products Administration (NMPA) has granted accelerated approval to rocbrutinib (development code: LP-168) for the treatment of adult patients with relapsed or refractory mantle cell lymphoma (R/R MCL) who have received at least two prior systemic therapies, including BTK inhibitors. (The Manila Times) - "Lupeng Pharmaceutical today announced that the National Medical Products Administration (NMPA) has granted accelerated approval to rocbrutinib (development code: LP-168) for the treatment of adult patients with relapsed or refractory mantle cell lymphoma (R/R MCL) who have received at least two prior systemic therapies, including BTK inhibitors...In April 2026, rocbrutinib was included for the first time in the Chinese Society of Clinical Oncology (CSCO) Guidelines for the Diagnosis and Treatment of Lymphoma , where it was listed as a Category II recommendation for the treatment of R/R MCL."

China approval • Clinical guideline • Mantle Cell Lymphoma

ROCKET-CLL: A randomized, open-label, multicenter, phase 3 study of rocbrutinib (LP-168) versus pirtobrutinib in covalent BTK inhibitor (cBTKi) in pretreated relapsed or refractory (R/R) chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL). (ASCO 2026) - P1, P3 | "Exploratory endpoints include health-related quality of life and biomarker assessment. Recruitment is ongoing."

Clinical • IO biomarker • P3 data • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Small Lymphocytic Lymphoma • TP53

A Study of Rocbrutinib Combined With R-GemOx in Patients With Relapsed or Refractory Diffuse Large B-cell Lymphoma (clinicaltrials.gov) - P1 | N=42 | Not yet recruiting | Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD.

New P1 trial • B Cell Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

ROCKET-CLL Global Phase 3 Study: Rocbrutinib vs Pirtobrutinib in cBTKi-Pretreated R/R CLL/SLL (clinicaltrials.gov) - P3 | N=306 | Recruiting | Sponsor: Newave Pharmaceutical Inc | Not yet recruiting ➔ Recruiting

Enrollment open • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma • BCL2 • TP53

Role of purine metabolism in CLL cell pathobiology and CLL disease progression (AACR 2024) - "But PNP inhibitor forodesine did not show any significant killing in high vs low/no PNP group. When we treated CLL cells from untreated patients with Bcl2 inhibitors venetoclax, S55746 and LP-118 (Bcl-2/Bcl-xl inhibitor, Newave), CLL cells showed increasing sensitivity to the Bcl2 inhibitors associated with their PNP expression (high>low>no PNP)...In contrast CLL cells when treated with both venetoclax and LP-168, showed more drug sensitivity in the high PNP expressing CLL cells vs low/no PNP. These results indicate that active purine metabolism in CLL cells can contribute to differential novel agent drug responses of CLL patients. Future studies to understand the exact mechanism of how PNP relates to this differential drug sensitivity should be instructive in regard to alternate maneuvers to treat CLL."

IO biomarker • Chronic Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Oncology • BCL2L1

A Study Evaluating the Effects of Itraconazole or Rifampin on the Pharmacokinetic Characteristics of Rocbrutinib Tablet (clinicaltrials.gov) - P1 | N=28 | Recruiting | Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD. | Not yet recruiting ➔ Recruiting

Enrollment open